Document Report Card

ID: ALA1138352

Journal: J Med Chem

Title: On the intractability of estrogen-related receptor alpha as a target for activation by small molecules.

Authors: Hyatt SM, Lockamy EL, Stein RA, McDonnell DP, Miller AB, Orband-Miller LA, Willson TM, Zuercher WJ.

Abstract: The estrogen-related receptor alpha (ERRalpha) is a potential target for activation in the treatment of metabolic disease. To date, no small-molecule agonists of ERRalpha have been identified despite several high-throughput screening campaigns. We describe the synthesis and profiling of a small array of compounds designed on the basis of a previously reported agonist-bound crystal structure of the closely related receptor ERRgamma. The results suggest that ERRalpha may be intractable as a direct target for pharmacologic activation.

CiteXplore: 18052088

DOI: 10.1021/jm7012387